题目：Single molecule based cancer specific targeting Drug Delivery System (DDS) 报告人：Prof. Jong Seung Kim Department of Chemistry, Korea University 地点：化学楼三楼报告厅 时间：2014年11月8号（星期六）上午10:00 联系人：张艳教授(njuzy@nju.edu.cn) We present the design, synthesis of a new type of targetable chemodosimetric fluorescent sensor for imaging hepatic thiols as well as for the drug delivery system. The in vivo and in vitro experimental results revealed that it selectively enters HepG2 cells as well as liver through ASGP-R-mediated endocytosis, and shows a fluorescence change. Thus, itis promising for the detection/imaging of hepaticthiollevels in vivoandfor the selective delivery of anticancer agent to the target cancer.The synthesis, spectroscopic characterization, and biological evaluation of a RGD peptide appended naphthalimide pro-CPT (1) are presented. Upon the disulfide bond cleavage reaction with free thiols, 1 displays a red-shifted fluorescence at535 nm and releases the CPT drug concomitantly in an aqueous solution at pH 7.4. Confocal microscopic experiments reveal that 1 is preferentially taken up by U87 cells over C6 cells and delivers the CPT drug through a RGD-dependent endocytosis. This new DDS system could provide a potential guideline for the construction of new therapeutic drug delivery and its monitoring system. 化学生物学与新药创制研究所 有机化学学科 |